US4863930AExpiredUtility

Use of substituted 5H-pyrido- and 5H-thiazolo(2',1':2,3)imidazo (4,5-b)indoles as cholinomimetic agents

Individually held — no corporate assignee on recordPriority: Dec 19, 1986Filed: Dec 19, 1986Granted: Sep 5, 1989
Est. expiryDec 19, 2006(expired)· nominal 20-yr term from priority
A61K 31/425A61K 31/44A61K 31/475
47
PatentIndex Score
16
Cited by
6
References
11
Claims

Abstract

5H-pyrido[2',1':2,3]imidazo[4,5-b]indoles of the formulae ##STR1## their pharmaceutically acceptable acid addition salts and the corresponding compounds bearing one or more halogens and/or lower-alkyl groups on the available ring carbon atoms are administered in cholinomimetic amounts to mammals with low acetylcholine or cholinergic activity to ameliorate the symptoms associated with that condition.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
       1. A method of treating a hypocholinergic mammal by ameliorating the symptoms associated with a cholinergic deficiency, which comprises administering a mammal in need thereof a therapeutically effective amount of a compound of one of the formulae ##STR3## or a pharmaceutically acceptable acid addition salt thereof, wherein R, R', R 1 , R' 1 , R 2 , R' 2 , R 3 , R' 3 , R 4 , R 5 , R 6  and R 7  each are hydrogen, halogen or lower-alkyl of from one to four carbon atoms, inclusive; R 8  is hydrogen or lower-alkyl of from one to four carbon atoms, inclusive; and R 9  is hydrogen or halo. 
     
     
       2. The method according to claim 1, wherein the mammal is a human being. 
     
     
       3. The method according to claim 1, wherein the compound is administered by injection. 
     
     
       4. The method according to claim 1, wherein the compound administered is a compound of Formula Ia or a pharmaceutically acceptable salt thereof. 
     
     
       5. The method according to claim 4, wherein R, R 1 , R 2  and R 3  collectively are 10-halo, 8,10-dihalo, 8,9-di-lower-alkyl or 7,9-di-lower-alkyl and R', R' 1 , R' 2 , and R' 3  collectively are 1-halo, 2-halo, 3-halo, 4-halo, 1-lower-alkyl, 2-lower-alkyl, 3-lower-alkyl, 4-lower-alkyl, 1,3-dihalo, 2,3-dihalo, 2,4-dihalo, 3,4-dihalo, 1,3-di-lower-alkyl, 2,3-di-lower-alkyl or 1,4-di-lower-alkyl. 
     
     
       6. The method according to claim 5, wherein the compound administered is 5H-pyrido[2',1':2,3]imidazo-[4,5-b]indole or a pharmaceutically acceptable salt thereof. 
     
     
       7. The method according to claim 6, wherein the mammal is a human being and wherein the compound is administered by injection. 
     
     
       8. The method according to claim 1, wherein the compound administered is a compound of Formula Ib or a pharmaceutically acceptable salt thereof. 
     
     
       9. The method according to claim 8, wherein R 4 , R 5 , R 6 , and R 7  collectively are 9-halo, 8-halo, 7-halo, 6-halo, 9-lower-alkyl, 8-lower-alkyl, 7-lower-alkyl, 6-lower-alkyl, 7,9-dihalo, 7,8-dihalo, 6,8-dihalo, 6,7-dihalo, 7,9-di-lower-alkyl, 7,8-di-lower-alkyl or 4,6-di-lower-alkyl. 
     
     
       10. The method according to claim 9, wherein the compound administered is 5H-thiazolo[2'1':2,3]imidazo-[4,5-b]indole or a pharmaceutically acceptable salt thereof. 
     
     
       11. The method according to claim 10, wherein the mammal is a human being and wherein the compound is administered by injection.

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